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Literature summary extracted from

  • Kumar, A.; Kawamura, T.; Kawatani, M.; Osada, H.; Zhang, K.
    Identification and structure-activity relationship of purine derivatives as novel MTH1 inhibitors (2017), Chem. Biol. Drug Des., 89, 862-869 .
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.6.1.56 (2Z)-2-methyl-4-[(9H-purin-6-yl)amino]but-2-en-1-ol
-
 Homo sapiens
3.6.1.56 2-chloro-6-(1,3,3-trimethyl-6-azabicyclo[3.2.1]octan-6-yl)-9H-purine
-
 Homo sapiens
3.6.1.56 2-[2-[(6-methoxy-3-methyl-1H-pyrazolo[3,4-b]quinolin-4-yl)amino]ethoxy]ethanol i.e. SCH-51344 Homo sapiens
3.6.1.56 6-(1,3,3-trimethyl-6-azabicyclo[3.2.1]octan-6-yl)-9H-purine
-
 Homo sapiens
3.6.1.56 6-(2,3-dichlorophenyl)-N4-methylpyrimidine-2,4-diamine i.e. TH287 Homo sapiens
3.6.1.56 N-(2-phenylethyl)-9H-purin-6-amine
-
 Homo sapiens
3.6.1.56 N-[(2H-1,3-benzodioxol-5-yl)methyl]-9H-purin-6-amine
-
 Homo sapiens
3.6.1.56 N-[(furan-2-yl)methyl]-9-methyl-9H-purin-6-amine
-
 Homo sapiens
3.6.1.56 N-[(furan-2-yl)methyl]-9H-purin-6-amine
-
 Homo sapiens
3.6.1.56 N-[3-[(propan-2-yl)oxy]propyl]-9H-purin-6-amine NPD15095, competitive inhibition Homo sapiens
3.6.1.56 N6-(2-methoxyethyl)-9H-purine-2,6-diamine
-
 Homo sapiens
3.6.1.56 N6-(2-phenylethyl)-9H-purine-2,6-diamine
-
 Homo sapiens
3.6.1.56 N6-benzyl-9H-purine-2,6-diamine
-
 Homo sapiens
3.6.1.56 N6-[2-(3,4-dimethoxyphenyl)ethyl]-9H-purine-2,6-diamine
-
 Homo sapiens
3.6.1.56 N6-[3-[(propan-2-yl)oxy]propyl]-9H-purine-2,6-diamine
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
3.6.1.56 2-hydroxy-dATP + H2O Homo sapiens
-
 2-hydroxy-dAMP + diphosphate
-
 ?
3.6.1.56 8-oxo-dGTP + H2O Homo sapiens
-
 8-oxo-dGMP + diphosphate
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
3.6.1.56 Homo sapiens P36639
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.6.1.56 2-hydroxy-dATP + H2O
-
 Homo sapiens 2-hydroxy-dAMP + diphosphate
-
 ?
3.6.1.56 8-oxo-dGTP + H2O
-
 Homo sapiens 8-oxo-dGMP + diphosphate
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.6.1.56 MTH1
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.6.1.56 0.00021
-
 with 8-oxo-dGTP as substrate, at pH 7.5, temperature not specified in the publication Homo sapiens 6-(1,3,3-trimethyl-6-azabicyclo[3.2.1]octan-6-yl)-9H-purine
3.6.1.56 0.00023
-
 with 8-oxo-dGTP as substrate, at pH 7.5, temperature not specified in the publication Homo sapiens 2-chloro-6-(1,3,3-trimethyl-6-azabicyclo[3.2.1]octan-6-yl)-9H-purine
3.6.1.56 0.00029
-
 with 8-oxo-dGTP as substrate, at pH 7.5, temperature not specified in the publication Homo sapiens N6-(2-phenylethyl)-9H-purine-2,6-diamine
3.6.1.56 0.00035
-
 with 2-hydroxy-dATP as substrate, at pH 7.5, temperature not specified in the publication Homo sapiens 2-chloro-6-(1,3,3-trimethyl-6-azabicyclo[3.2.1]octan-6-yl)-9H-purine
3.6.1.56 0.00038
-
 with 2-hydroxy-dATP as substrate, at pH 7.5, temperature not specified in the publication Homo sapiens 6-(1,3,3-trimethyl-6-azabicyclo[3.2.1]octan-6-yl)-9H-purine
3.6.1.56 0.00042
-
 with 2-hydroxy-dATP as substrate, at pH 7.5, temperature not specified in the publication Homo sapiens N6-[2-(3,4-dimethoxyphenyl)ethyl]-9H-purine-2,6-diamine
3.6.1.56 0.0005
-
 with 2-hydroxy-dATP as substrate, at pH 7.5, temperature not specified in the publication Homo sapiens N6-(2-phenylethyl)-9H-purine-2,6-diamine
3.6.1.56 0.00063
-
 with 8-oxo-dGTP as substrate, at pH 7.5, temperature not specified in the publication Homo sapiens N6-benzyl-9H-purine-2,6-diamine
3.6.1.56 0.00113
-
 with 2-hydroxy-dATP as substrate, at pH 7.5, temperature not specified in the publication Homo sapiens N6-benzyl-9H-purine-2,6-diamine
3.6.1.56 0.0019
-
 with 8-oxo-dGTP as substrate, at pH 7.5, temperature not specified in the publication Homo sapiens N6-[3-[(propan-2-yl)oxy]propyl]-9H-purine-2,6-diamine
3.6.1.56 0.0028
-
 with 2-hydroxy-dATP as substrate, at pH 7.5, temperature not specified in the publication Homo sapiens N6-[3-[(propan-2-yl)oxy]propyl]-9H-purine-2,6-diamine
3.6.1.56 0.0028
-
 with 8-oxo-dGTP as substrate, at pH 7.5, temperature not specified in the publication Homo sapiens N-(2-phenylethyl)-9H-purin-6-amine
3.6.1.56 0.00333
-
 with 8-oxo-dGTP as substrate, at pH 7.5, temperature not specified in the publication Homo sapiens N-[3-[(propan-2-yl)oxy]propyl]-9H-purin-6-amine
3.6.1.56 0.0039
-
 with 2-hydroxy-dATP as substrate, at pH 7.5, temperature not specified in the publication Homo sapiens N-(2-phenylethyl)-9H-purin-6-amine
3.6.1.56 0.0048
-
 with 8-oxo-dGTP as substrate, at pH 7.5, temperature not specified in the publication Homo sapiens N6-(2-methoxyethyl)-9H-purine-2,6-diamine
3.6.1.56 0.0067
-
 with 2-hydroxy-dATP as substrate, at pH 7.5, temperature not specified in the publication Homo sapiens N-[3-[(propan-2-yl)oxy]propyl]-9H-purin-6-amine
3.6.1.56 0.0091
-
 with 2-hydroxy-dATP as substrate, at pH 7.5, temperature not specified in the publication Homo sapiens N6-(2-methoxyethyl)-9H-purine-2,6-diamine
3.6.1.56 0.014
-
 with 8-oxo-dGTP as substrate, at pH 7.5, temperature not specified in the publication Homo sapiens (2Z)-2-methyl-4-[(9H-purin-6-yl)amino]but-2-en-1-ol
3.6.1.56 0.02
-
 with 8-oxo-dGTP as substrate, at pH 7.5, temperature not specified in the publication Homo sapiens N-[(2H-1,3-benzodioxol-5-yl)methyl]-9H-purin-6-amine
3.6.1.56 0.02
-
 with 8-oxo-dGTP as substrate, at pH 7.5, temperature not specified in the publication Homo sapiens N-[(furan-2-yl)methyl]-9H-purin-6-amine
3.6.1.56 0.021
-
 with 8-oxo-dGTP as substrate, at pH 7.5, temperature not specified in the publication Homo sapiens N6-[2-(3,4-dimethoxyphenyl)ethyl]-9H-purine-2,6-diamine
3.6.1.56 0.022
-
 with 2-hydroxy-dATP as substrate, at pH 7.5, temperature not specified in the publication Homo sapiens (2Z)-2-methyl-4-[(9H-purin-6-yl)amino]but-2-en-1-ol
3.6.1.56 0.028
-
 with 2-hydroxy-dATP as substrate, at pH 7.5, temperature not specified in the publication Homo sapiens N-[(2H-1,3-benzodioxol-5-yl)methyl]-9H-purin-6-amine
3.6.1.56 0.029
-
 with 2-hydroxy-dATP as substrate, at pH 7.5, temperature not specified in the publication Homo sapiens N-[(furan-2-yl)methyl]-9H-purin-6-amine
3.6.1.56 1
-
 IC50 above 1.0 mM, with 8-oxo-dGTP as substrate, at pH 7.5, temperature not specified in the publication Homo sapiens N-[(furan-2-yl)methyl]-9-methyl-9H-purin-6-amine

General Information

EC Number General Information Comment Organism
3.6.1.56 physiological function the enzyme prevents the incorporation of oxidized nucleotides such as 2-hydroxy-ATP and 8-oxo-dGTP during DNA replication by hydrolysing them into their corresponding monophosphates Homo sapiens